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(+)-N-Allylnormetazocine hydrochloride

Cat. No. M28180
(+)-N-Allylnormetazocine hydrochloride Structure
Synonym:

(+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride

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Biological Activity

(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease.

Chemical Information
Molecular Weight 293.83
Formula C17H24ClNO
CAS Number 133005-41-1
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Mohan Pabba, et al. J Neurosci. NMDA receptors are upregulated and trafficked to the plasma membrane after sigma-1 receptor activation in the rat hippocampus

[2] S Shimazu, et al. Eur J Pharmacol. sigma receptor ligands attenuate N-methyl-D-aspartate cytotoxicity in dopaminergic neurons of mesencephalic slice cultures

[3] K Ishiwata, et al. Nucl Med Biol. In vivo binding of [11C]nemonapride to sigma receptors in the cortex and cerebellum

[4] D W Bonhaus, et al. J Pharmacol Exp Ther. [3H]RS-23597-190, a potent 5-hydroxytryptamine4 antagonist labels sigma-1 but not sigma-2 binding sites in guinea pig brain

[5] M Volonté, et al. J Pharmacol Exp Ther. Effect of the 5-hydroxytryptamine3 receptor antagonist itasetron (DAU 6215) on (+)-N-allylnormetazocine-induced dopamine release in the nucleus accumbens and in the corpus striatum of the rat: an in vivo microdialysis study

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Keywords: (+)-N-Allylnormetazocine hydrochloride, (+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride supplier, Opioid Receptor, inhibitors, activators

 
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